CN1660865A - Baishouwu saponin compounds, total saponins and their application in drugs for treating gastrointestinal diseases - Google Patents
Baishouwu saponin compounds, total saponins and their application in drugs for treating gastrointestinal diseases Download PDFInfo
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- CN1660865A CN1660865A CN 200410099270 CN200410099270A CN1660865A CN 1660865 A CN1660865 A CN 1660865A CN 200410099270 CN200410099270 CN 200410099270 CN 200410099270 A CN200410099270 A CN 200410099270A CN 1660865 A CN1660865 A CN 1660865A
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- radix
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- saponin
- glycosides
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- 150000002338 glycosides Chemical class 0.000 claims description 85
- 229930002600 steroidal saponin Natural products 0.000 claims description 59
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Abstract
7 C12 steroid saponins including white fleeceflower glucosides A, B and C, white fleeceflower neoglucosides A and B, etc, and their mixture is prepared from white fleeceflower root. They can be used to prevent and treat gastrosis, gastric ulcer and duodenal ulcer.
Description
Technical field
The invention belongs to medical technical field, the mixture (radix cynanchi bungei total saponin(e) that is specifically related to a kind of saponins compound that extraction separation obtains from the Chinese medicine Root of Bunge Auriculate and contains this saponins compound, and the application in the medicine of diseases such as prevention and treatment gastric duodenal ulcer, gastritis, stomach and bowel movement obstacle.
Background technology
Root of Bunge Auriculate is the piece root of asclepiadaceae (Asclepiadaceae) Cynanchum plant Auriculoside A (Cynanchum auriculatumRoyle ex Wight.), Bunge Swallowwort Root (Cynanchum bungei Decne.), Root of Wilford Swallowwort (Cynanchum wilfordii (Maxim.) Hemsl.), Root of Bunge Auriculate has nourishing liver and replenishing blood, reinforces the kidney that benefit is smart, the effect of strengthening the muscles and bones in the theory of traditional Chinese medical science, and have the function of invigorating the spleen and benefiting QI concurrently, be used for the treatment of diseases such as strong, the uncomfortable in chest pained and maldigestion of insomnia forgetfulness, early whitening of beard and hair, muscles and bones.
Root of Bunge Auriculate has the effect of food digesting stomach fortifying, regulating QI to relieve pain, the diffusing joint of detumescence in Tujia and Miao ethnic group's national medicine theory, is used for the treatment of diseases such as gastroenteritis, maldigestion.
Summary of the invention
The objective of the invention is, according to Tujia, Miao ethnic group's national medicine theory and treatment experience, in conjunction with modern chemistry and pharmacology means, the saponins compound and the radix cynanchi bungei total saponin(e of extraction separation high-efficiency low-toxicity, treatment gastrointestinal tract disease from Root of Bunge Auriculate.
The present invention's extraction separation from Root of Bunge Auriculate has the saponins compound of treatment gastrointestinal tract disease effect, obtain 7 kinds of carbon-21 steroidal saponin(es, be respectively: Root of Bunge Auriculate glycosides A, Root of Bunge Auriculate glycosides B, Root of Bunge Auriculate glycosides C, the new glycosides A of Root of Bunge Auriculate, the new glycosides B of Root of Bunge Auriculate, Auriculoside A glycosides A, Auriculoside A glycosides B, and mixture---the radix cynanchi bungei total saponin(e that comprises this 1-7 kind carbon-21 steroidal saponin(e.In this total saponins, the weight content of its saponin compound 〉=50% usually
Root of Bunge Auriculate saponins compound and total saponins that the present invention extracts can be used for treating gastritis, gastrointestinal ulceration, gastrointestinal tract dyskinesis, pains and other diseases, have characteristics such as high-efficiency low-toxicity and the recurrence of minimizing gastrointestinal tract disease.It is the new drug of the conduct treatment gastrointestinal tract disease that extraction separation obtains from natural resource.
Experimental results show that, above-mentioned these carbon-21 steroidal saponin(es, and the mixture radix cynanchi bungei total saponin(e that includes these carbon-21 steroidal saponin(es, it is all inhibited that the impatient gastric ulcer of stress in rats, pyloric ligation ulcers acute gastric ulcer, acetate are burnt the drug-induced stomach ulcer of type chronic gastric ulcer, hot branded type chronic gastric ulcer, subcutaneous injection of reserpine, mercaptoethylamine inductive rat preduodenal ulcer, rat superficial gastritis etc., can reduce ulcer and hemorrhage incidence, average ulcer area and hemorrhage area are reduced; Secretion to rat gastric juice and hydrochloric acid in gastric juice is inhibited; Gastric mucosa injury to the manufacturing of rat oral aspirin has provide protection; Hp to vitro culture has killing action; Inflammatory pain to the manufacturing of rats by intraperitoneal injection strong acid has analgesic activity; Irritate stomach at rat ethanol and cause in the gastric mucosa injury, can reduce the stomach mucous membrane lipid peroxide contents, gastric mucosa injury due to the oxyradical is had provide protection; And can promote rat stomach evacuation rate and rat intestine wriggling.
7 kinds of carbon-21 steroidal saponin(es among the present invention are 7 kinds of glucosides that a kind of and different quantities among 3 kinds of steroid sapogenin caudatin, kidiolanin shown in following 3 chemical structures, the metaplexigenin, dissimilar sugar form, and wherein R is a sugar chain:
caudatin????????????????????????????????????kidiolanin?????????????????????????????????metaplexigenin
Among the Root of Bunge Auriculate glycosides A, aglycon is kidiolanin (kidjolanin), and R is the lucky pyrans of β-D-glucopyanosyl base-(1 → 4)-α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-α-L-enlightening glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Among the Root of Bunge Auriculate glycosides B, aglycon is metaplexigenin (a periplocin unit), and R is the lucky pyrans of α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-α-L-enlightening glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Among the Root of Bunge Auriculate glycosides C, aglycon is caudatin (announcement reaches booth), and R is the lucky pyrans of β-D-glucopyanosyl base-(1 → 4)-β-L-glucopyanosyl base-(1 → 4)-α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranose-(1 → 4)-α-L-enlightening glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Among the new glycosides A of Root of Bunge Auriculate, aglycon is caudatin (announcement reaches booth), and R is β-D-glucopyanosyl base-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Among the new glycosides B of Root of Bunge Auriculate, aglycon is caudatin (announcement reaches booth), and R is β-D-glucopyanosyl base-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-digoxigenin pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Among the Auriculoside A glycosides A, aglycon is caudatin (announcement reaches booth), and R is β-D-glucopyanosyl base-(1 → 4)-α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Among the Auriculoside A glycosides B, aglycon is caudatin (announcement reaches booth), and R is β-D-glucopyanosyl base-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-digoxigenin pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Carbon-21 steroidal saponin(e provided by the invention and to include the preparation method of mixture radix cynanchi bungei total saponin(e of carbon-21 steroidal saponin(e as follows: Root of Bunge Auriculate is extracted as extracting solvent with ethanol etc., extracting solution is concentrated the medicinal extract that obtains, separate through macroporous resin column chromatography again, collect ethanol eluate, concentrate, promptly obtain the radix cynanchi bungei total saponin(e.To total saponins through silica gel column chromatography, detect the chromatography flow point with thin-layer chromatography, flow point with identical single spot merges, concentrate, separate and purifying through RP-18 lower pressure column or HPLC (high performance liquid chromatography) again, get Root of Bunge Auriculate glycosides A, Root of Bunge Auriculate glycosides B, Root of Bunge Auriculate glycosides C, the new glycosides A of Root of Bunge Auriculate, the new glycosides B of Root of Bunge Auriculate, Auriculoside A glycosides A, Auriculoside A glycosides B.
By spectral analysis techniques such as acid hydrolysis and ultraviolet spectrometer, infrared spectrometer, high resolution fast atom bombardment MS instrument, hydrogen nuclear magnetic resonance spectrometer, carbon-13 nmr spectra instrument, the relevant spectrometer of heteronuclear volume, the relevant spectrometers of heteronuclear multikey, obtain the chemical structure of above-mentioned 7 kinds of carbon-21 steroidal saponin(es, be followed successively by: the lucky pyrans of kidiolanin (kidjolanin)-β-D-glucopyanosyl base-(1 → 4)-α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-α-L-enlightening glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside; The lucky pyrans of metaplexigenin (periplocin unit)-α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-α-L-enlightening glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside; Caudatin (announcement reaches booth)-be the lucky pyrans of β-D-glucopyanosyl base-(1 → 4)-β-L-glucopyanosyl base-(1 → 4)-α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranose-(1 → 4)-α-L-enlightening glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside; Caudatin (announcement reaches booth)-β-D-glucopyanosyl base-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside; Caudatin (announcement reaches booth)-β-D-glucopyanosyl base-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-digoxigenin pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside; Caudatin (announcement reaches booth)-β-D-glucopyanosyl base-(1 → 4)-α-L-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside; Caudatin (announcement reaches booth)-β-D-glucopyanosyl base-(1 → 4)-β-D-Apocynum cannabinum pyrans glycosyl-(1 → 4)-β-D-Folium seu Cortex Nerii pyrans glycosyl-(1 → 4)-β-D-digoxigenin pyrans glycosyl-(1 → 4)-β-D-Apocynum cannabinum pyranoside.
Root of Bunge Auriculate saponins compound provided by the invention and total saponins can be used for preparing the new drug for the treatment of gastrointestinal tract disease.According to the significant quantity of anti-gastrointestinal tract disease and acceptable carrier pharmaceutically, form pharmaceutical composition.Make various preparations, comprise tablet, granule, capsule, oral liquid, dripping pill, mixture, solution, syrup, tincture, injection.
Radix cynanchi bungei total saponin(e among the present invention and 7 compounds have been carried out the active evaluation experimental of anti-gastric-ulcer.
(1) Root of Bunge Auriculate carbon-21 steroidal saponin(e Chinese People's Anti-Japanese Military and Political College mouse irritability acute gastric ulcer effect.
1. method
The index of ulcer replication of Model and ulcer level: select the SD rat for use, male and female half and half, body weight 200-250g, animal is divided into 24 experimental group at random, 1 famotidine group and 1 blank group.Fasting 24h before the experiment freely drinks water.Experimental group in immersion stress before 30min distinguish 7 carbon-21 steroidal saponin(es of ig (10mg/kg, 20mg/kg, 40mg/kg), the radix cynanchi bungei total saponin(e (50mg/kg, 100mg/kg, 200mg/kg), volume 10mL/kg (down together), all (carboxymethyl cellulose, CMC) solution is made into desired concn with the 5g/L carboxymethyl cellulose with preceding for famotidine group ig famotidine (100mg/kg), above medicine.The physiological saline of blank group ig respective volume.Water temperature (23 ± 1) ℃, immersion stress 5h, put to death animal, observe the ulcer situation.Press the method for Cuth and calculate ulcer index.
Data processing: data are with mean ± standard deviation (x ± SD) expression.According to every group of ulcer index of gained, the calculation formula of pressing ulcer inhibition rate: ulcer inhibition rate=[(control group index-administration class index)/control group index] * 100%; Calculate ulcer inhibition rate.The relatively employing t check of each group difference.
2 results
7 carbon-21 steroidal saponin(es of ig and radix cynanchi bungei total saponin(e (10-40mg/kg) can obviously suppress the formation (table 1) of the impatient gastric ulcer of stress in rats.
7 carbon-21 steroidal saponin(es of table 1 ig and radix cynanchi bungei total saponin(e are to the influence of the impatient gastric ulcer of stress in rats
| Group | Dosage (mg/kg) | Number of animals | Ulcer index | Ulcer inhibition rate (%) |
| Blank famotidine group cynauricuoside A cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B | ????- ????100 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 | ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 | ????48.52±7.32 ????8.33±4.01** ????25.69±8.11* ????18.44±4.69** ????11.06±6.85** ????28.19±5.18* ????24.44±7.61* ????10.76±6.77** ????31.69±9.21 ????26.44±6.60* ????13.46±6.15** ????22.55±8.71* ????13.07±4.39** ????10.96±7.85** ????26.49±7.01* ????21.54±6.91* ????12.06±5.25** ????31.32±8.85 ????24.54±8.69* ????12.06±6.24** ????24.75±6.51* ????15.44±4.69** | ????- ????83.91** ????47.20* ????63.06** ????88.71** ????44.15* ????52.33* ????81.09** ????38.25 ????48.65* ????74.24** ????56.13* ????74.51** ????80.16** ????48.63* ????51.97* ????76.35** ????37.89 ????51.48* ????76.69** ????51.84* ????71.24** |
| Group | Dosage (mg/kg) | Number of animals | Ulcer index | Ulcer inhibition rate (%) |
| The radix cynanchi bungei total saponin(e | ????40 ????50 ????100 ????200 | ????10 ????10 ????10 ????10 | ????10.22±6.35** ????31.54±8.06 ????25.07±6.19* ????13.06±8.27** | ????79.32** ????38.14 ????49.56* ????74.35** |
Compare with the blank group: * P＜0.05, * * P＜0.01
(2) Root of Bunge Auriculate carbon-21 steroidal saponin(e Chinese People's Anti-Japanese Military and Political College mouse pyloric ligation ulcers acute gastric ulcer effect.
1. method
The Wister rat, body weight 250g ± 30g, male and female half and half.Animal is divided into 24 experimental group at random, 1 famotidine control group and 1 blank group.Experimental group is 7 carbon-21 steroidal saponin(es of ig (10mg/kg respectively, 20mg/kg, 40mg/kg), the radix cynanchi bungei total saponin(e (50mg/kg, 100mg/kg, 200mg/kg), volume 10mL/kg (down together), all (carboxymethylcellulose, CMC) solution is made into desired concn with the 5g/L carboxymethyl cellulose with preceding for famotidine group ig famotidine (100mg/kg), above medicine.The physiological saline of blank group ig respective volume.Above-mentioned respectively the group irritated stomach every day 1 time by measure, and 15d respectively organizes and all supplies with normal diet continuously.Each organizes fasting 48h after the last administration, uses pylorus ligature law, makes gastric ulcer model.Concrete operations are: under the big white mouse general anesthesia state, aseptic technique is opened the abdominal cavity along ventrimeson, and the ligation pylorus is sewed up stomach wall, and postoperative is with the animal sub-cage rearing.Sacrificed by decapitation animal behind the 19h is then with the fixing stomach sample of 1% formaldehyde solution.Cut open inspection behind the 30min, calculate ulcer index.
Data processing: data are with mean ± standard deviation (x ± SD) expression.According to every group of ulcer index of gained, the calculation formula of pressing ulcer inhibition rate: ulcer inhibition rate=[(control group index-administration class index)/control group index] * 100%; Calculate ulcer inhibition rate.The relatively employing t check of each group difference.
2. result
Dissect the back and find to have in the blank group 3 examples that the stomach ulcer perforation takes place, other each groups are not seen perforation, and 7 carbon-21 steroidal saponin(es of ig and radix cynanchi bungei total saponin(e (10-40mg/kg) can obviously suppress the formation (table 2) of rat pyloric ligation ulcers acute gastric ulcer.
7 carbon-21 steroidal saponin(es of table 2 ig and radix cynanchi bungei total saponin(e are to the influence of rat pyloric ligation ulcers acute gastric ulcer
| Group | Dosage (mg/kg) | Number of animals | Ulcer index | Ulcer inhibition rate (%) |
| Blank famotidine group Root of Bunge Auriculate glycosides A | ????- ????100 ????10 ????20 | ????10 ????10 ????10 ????10 | ????45.52±6.10 ????8.05±4.02** ????24.61±7.13* ????17.24±5.29** | ????- ????83.24** ????47.58* ????63.25** |
| Group | Dosage (mg/kg) | Number of animals | Ulcer index | Ulcer inhibition rate (%) |
| Cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????50 ????100 ????200 | ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 | ??12.06±6.75** ??27.19±6.08* ??25.44±6.90* ??11.76±5.27** ??32.65±8.01 ??25.24±5.96* ??12.76±5.15** ??23.15±9.31* ??12.47±8.09** ??10.46±6.55** ??26.39±7.91* ??23.84±6.68* ??12.28±5.69** ??33.92±7.65 ??24.04±8.11* ??13.11±7.64** ??28.75±6.28* ??14.40±5.09** ??11.92±5.15** ??32.94±9.07 ??25.57±6.88* ??12.06±8.54** | ??83.32** ??40.57* ??44.42* ??85.65** ??38.97 ??46.07* ??82.51** ??48.61* ??83.35** ??77.84** ??42.69* ??41.26* ??83.76** ??25.70 ??46.95* ??82.14** ??36.90* ??78.05** ??74.85** ??25.63 ??44.22* ??84.21** |
Compare with the blank group: * P＜0.05, * * P＜0.01
(3) Root of Bunge Auriculate carbon-21 steroidal saponin(e Chinese People's Anti-Japanese Military and Political College mouse acetate burns the effect of type chronic gastric ulcer.
1 method
Make and touch and divide into groups: get the SD rat, male and female half and half, body weight 200-250g.The conventional raising, and irrigate stomach by 10g/kg with 10% rheum officinale decocting liquid, 1 time/d, continuous 10 days.The back is injected under the gastric gland portion serous coat with microsyringe, to form papule degree of being with 20% acetate 0.1mL.With opening abdomen behind the etherization, expose full stomach before the art.Postoperative is sewed up stomach wall, the sterilization wound. the conventional raising.Postoperative next day, animal is divided into 24 experimental group at random, 1 Cimitidine Type A/AB control group and 1 blank group.
Index is collected: after rat is pressed above-mentioned grouping, use 7 carbon-21 steroidal saponin(es of ig (5mg/kg respectively, 10g/kg, 20mg/kg) with radix cynanchi bungei total saponin(e (50mg/kg, 100mg/kg, 200mg/kg), medicine control group ig Cimitidine Type A/AB (100mg/kg), all (carboxymethyl cellulose, CMC) solution is made into desired concn to above medicine with the 5g/L carboxymethyl cellulose with preceding.Blank group ig distilled water (10mL/kg).1 time/d, continuous 14 days.Put to death rat on the 15th day, get stomach after, cut off along greater gastric curvature, the flushing gastric content is put in 1% formaldehyde solution and is fixed 5 minutes.Stomach is open and flat on plank, present the ulcer index with ulcer number, ulcer area, evaluation that magnifying glass is observed and measured on the stomach mucous membrane, calculate ulcer inhibition rate.
2. result
7 carbon-21 steroidal saponin(es of ig and radix cynanchi bungei total saponin(e (10-40mg/kg) can obviously suppress the formation (table 3) that rats acetic acid burns the type chronic gastric ulcer.
7 carbon-21 steroidal saponin(es of table 3 ig and radix cynanchi bungei total saponin(e burn the influence of type chronic gastric ulcer to rats acetic acid
| Group | Dosage (mg/kg) | Number of animals | Ulcer index | Ulcer inhibition rate |
| Blank Cimetidine group cynauricuoside A cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????- ????100 ????5 ????10 ????20 ????5 ????10 ????20 ????5 ????10 ????20 ????5 ????10 ????20 ????5 ????10 ????20 ????5 ????10 ????20 ????5 ????10 ????20 ????50 ????100 ????200 | ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 | ????47.63±7.25 ????8.35±4.02** ????24.61±7.13* ????17.24±5.29** ????12.06±6.75** ????27.19±6.08* ????25.44±6.90* ????11.76±5.27** ????32.65±8.01 ????25.24±5.96* ????12.76±5.15** ????23.15±9.31* ????12.47±8.09** ????10.46±6.55** ????26.39±7.91* ????23.84±6.68* ????12.28±5.69** ????33.92±7.65 ????24.04±8.11* ????13.11±7.64** ????28.75±6.28* ????14.40±5.09** ????11.92±5.15** ????32.94±9.07 ????25.57±6.88* ????12.06±8.54** | ????- ????82.71** ????41.73* ????62.87** ????74.69** ????42.19* ????45.93* ????74.91** ????31.08 ????47.40* ????72.76** ????50.11* ????74.45** ????81.79** ????44.78* ????49.78* ????73.82** ????27.90 ????48.94* ????72.18** ????48.72* ????69.28** ????74.73** ????30.64 ????45.52* ????73.58** |
Compare with the blank group: * P＜0.05, * * P＜0.01
(4) the drug-induced stomach ulcer effect of the anti-mouse of Root of Bunge Auriculate carbon-21 steroidal saponin(e.
1 method
Kunming mouse, body weight 18～20g, male and female half and half, animal is divided into 24 experimental group at random, 1 positive controls and 1 blank group, 10 every group.7 carbon-21 steroidal saponin(es of experimental group ig (10mg/kg, 20mg/kg, 40mg/kg), the radix cynanchi bungei total saponin(e (50mg/kg, 100mg/kg, 200mg/kg), volume 10mL/kg (down together), all (carboxymethyl cellulose, CMC) solution is made into desired concn with the 5g/L carboxymethyl cellulose with preceding for positive controls ig Cimitidine Type A/AB (100mg/kg), above medicine.The physiological saline of blank group ig respective volume.Gastric infusion, every day 1 time, continuous 7 days.After after the last administration 1 hour, abdominal injection serpentine 5mg/kg put to death mouse after 18 hours, and stomach is taken out in operation, the point-like ulcer number (experimental result sees Table 4) that every mouse coat of the stomach of test under microscope produces.
2. result
7 carbon-21 steroidal saponin(es of ig and radix cynanchi bungei total saponin(e can obviously suppress the formation (table 4) of the drug-induced stomach ulcer of mouse.
7 carbon-21 steroidal saponin(es of table 4 ig and radix cynanchi bungei total saponin(e are to the influence of the drug-induced stomach ulcer of mouse
| Group | Dosage (mg/kg) | Number of animals | Ulcer quantity (individual) | Ulcer inhibition rate (%) |
| Blank Cimetidine group cynauricuoside A cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A | ????- ????100 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 | ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 | ????39.52±7.13 ????10.36±4.02** ????24.71±7.13* ????17.24±5.29** ????12.06±7.76** ????27.19±7.08* ????25.44±6.90* ????11.77±7.27** ????32.65±8.01 ????27.24±5.96* ????12.77±6.15** ????23.17±9.31* ????12.47±8.09** ????10.46±7.56** ????27.39±7.91* ????23.84±6.78* ????12.28±6.79** ????33.92±7.67 ????24.04±8.11* ????13.11±7.64** | ????74.52** ????39.25* ????57.36** ????69.54** ????22.39* ????37.54* ????61.98** ????19.56 ????32.14* ????68.14** ????42.26* ????69.06** ????74.85** ????31.59* ????40.87* ????69.25** ????26.50 ????40.36* ????66.42** |
| Group | Dosage (mg/kg) | Number of animals | Ulcer quantity (individual) | Ulcer inhibition rate (%) |
| Auriculoside A glycosides B radix cynanchi bungei total saponin(e | ????10 ????20 ????40 ????60 ????100 ????200 | ????10 ????10 ????10 ????10 ????10 ????10 | ????28.77±6.28* ????14.40±7.09** ????11.92±5.16** ????32.94±9.07 ????27.67±6.88* ????12.07±8.64** | ????28.24* ????66.58** ????71.58** ????11.54 ????31.05* ????69.51** |
Compare with the blank group: * P＜0.05, * * P＜0.01
(5) Root of Bunge Auriculate carbon-21 steroidal saponin(e suppresses the effect of rat gastric juice and gastric acid secretion.
1. method
The SD rat, male and female half and half, body weight (240 soil 10) g.Rat is divided into 24 experimental group at random, 1 famotidine group and 1 blank group.7 carbon-21 steroidal saponin(es of experimental group ig (10mg/kg, 20mg/kg, 40mg/kg), the radix cynanchi bungei total saponin(e (50mg/kg, 100mg/kg, 200mg/kg), all (carboxymethyl cellulose, CMC) solution is made into desired concn to above medicine with the 5g/L carboxymethyl cellulose with preceding.Control rats such as gavages at the medicine or the equal-volume CMC solution of capacity, continuously 3d.With the rat of fasting 24h, the row pyloric ligation, and duodenal administration is once, water is prohibited in the postoperative fasting, puts to death animal behind the 4h, collects gastric juice in graduated centrifuge tube.Simultaneously cut off stomach along greater gastric curvature, turn up, go the free mucus of gastric mucosa surface with PH5.8 citric acid-phosphate buffered saline buffer flushing, again stomach is immersed in the 10mL 0.2g/L A Erxinlan liquid, put 25 ℃ of incubation 2h, take out stomach,, get supernatant liquor 615nm place colorimetric with the centrifugal A Erxinlan liquid of 2500r/min 10min.Get gastric juice 0.1mL and put test tube, add 10g/L A Erxinlan solution 0.1mL, PH5.8 citric acid-phosphate buffered saline buffer 3.3mL, distilled water 0.6mL, abundant mixing, room temperature 24h, 2500r/min centrifugal reaction solution 10min gets supernatant liquor 615nm place colorimetric, measures residue A Erxinlan liquid measure.The centrifugal 10min of all the other gastric juice 2000r/min measures gastric juice amount, total acidity, total acid output, stomach en-output respectively.The acid base neutralization titration method is adopted in gastric acidity determination.
2. result
7 carbon-21 steroidal saponin(es and radix cynanchi bungei total saponin(e can obviously reduce the rat gastric secretion; And rat gastric juice total acid output and stomach en-output all there is obvious suppression.
Table 5 Root of Bunge Auriculate carbon-21 steroidal saponin(e suppresses the influence of rat gastric juice and gastric acid secretion
| Group | Dosage (mg/kg) | Gastric juice amount (mL) | Stomach total acid content (mmol/L) | The total acid output of stomach (mmol/Lh) | Stomach en-output (U/h) |
| Blank group famotidine group Root of Bunge Auriculate glycosides A | ????- ????100 ????10 ????20 ????40 | ????9.52±3.43 ????2.36±1.02** ????6.71±2.13* ????3.24±2.29** ????2.06±1.76** | ????84.72±31.50 ????40.16±24.82** ????64.51±27.13* ????34.24±15.29** ????35.66±17.76** | ????138.52±50.11 ????51.35±20.32** ????80.01±40.13* ????65.20±65.28** ????60.35±30.05** | ????486.59±179.43 ????214.37±125.42** ????325.61±157.13* ????217.25±125.26** ????225.47±130.47** |
| Group | Dosage (mg/kg) | Gastric juice amount (mL) | Stomach total acid content (mmol/L) | The total acid output of stomach (mmol/Lh) | Stomach en-output (U/h) |
| Cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????60 ????100 ????200 | ????7.19±3.08* ????5.44±2.90* ????1.97±1.27** ????8.65±4.01 ????7.24±3.96* ????2.77±1.15** ????6.17±3.31* ????3.47±2.09** ????2.46±1.56** ????6.39±3.91* ????5.84±2.78* ????2.28±1.79** ????8.92±3.67 ????5.04±3.11* ????2.11±1.64** ????5.77±3.28* ????2.40±1.09** ????1.92±1.16** ????8.94±4.07 ????6.67±3.88* ????3.07±1.64** | ????67.79±27.08* ????55.84±26.90* ????31.57±17.27** ????72.15±28.01 ????57.64±25.96* ????32.27±16.15** ????53.97±29.31* ????40.17±18.09** ????31.36±17.56** ????58.89±27.91* ????41.24±26.78* ????32.08±16.79** ????73.52±27.67 ????54.04±28.11* ????33.91±17.64** ????58.73±26.28* ????34.30±17.09** ????31.02±15.16** ????75.54±29.73 ????57.87±26.88* ????32.27±18.64** | ??94.18±40.38* ??75.00±35.83* ??51.00±20.20** ??120.55±58.31 ??70.20±45.85* ??52.00±35.15** ??63.10±38.31* ??52.00±28.38** ??43.05±20.55** ??90.38±30.81* ??73.80±35.08* ??52.28±25.08** ??123.82±50.50 ??97.30±48.12* ??69.18±30.50** ??85.40±45.28* ??75.03±30.38** ??53.82±25.15** ??113.58±58.30 ??85.50±45.88* ??62.34±38.50** | ??297.16±157.48* ??325.55±186.64* ??201.86±125.29** ??382.75±198.41 ??307.25±165.67* ??262.64±170.15** ??243.17±116.31* ??192.57±98.46** ??214.57±104.57** ??349.36±197.61* ??303.85±167.08* ??212.28±127.86** ??393.62±200.87 ??342.45±218.14* ??253.11±187.65** ??328.47±137.28* ??215.54±147.46** ??211.62±95.17** ??382.65±186.67 ??327.07±126.88* ??242.46±98.75** |
Compare with the blank group: * P＜0.05, * * P＜0.01
(6) Root of Bunge Auriculate carbon-21 steroidal saponin(e is to the restraining effect of vitro culture Hp (HP).
1. method
The preparation of Root of Bunge Auriculate carbon-21 steroidal saponin(e concentration: the carbon-21 steroidal saponin(e is dissolved in the aseptic carboxymethyl cellulose of 4.65ml (5g/L) solution, doubling dilution then, its concentration are respectively 1,0.5,0.25,0.125,0.0625,0.0313,0.0156,0.0078,0.0039g/mL.Use the plate punch method then, evenly be coated with HP on rabbit blood culture-medium,, the tested medicine of above-mentioned different concns is directly added in the hand-hole with the corneal trephine punching of diameter 5.5mm.Little aerobic environment is cultivated 72h for 37 ℃.Measure antibacterial circle diameter, obtain inhibiting rate and minimum inhibitory concentration.
2. result
From experimental result, Root of Bunge Auriculate carbon-21 steroidal saponin(e has certain bacteriostatic action to HP external, and minimum inhibitory concentration (MIC) is 0.0156g/mL.
The external restraining effect of table 6 Root of Bunge Auriculate carbon-21 steroidal saponin(e (inhibiting rate %) to Hp (HP)
| Group | Concentration (g/mL) |
| ????1 | ????0.5 | ????0.25 | ????0.125 | ????0.0625 | ????0.0313 | ????0.0156 | |
| The blank group | ????- | ????- | ????- | ????- | ????- | ????- | ????- |
| The amoxycilline Trihydrate bp group | ????92 | ????89 | ????75 | ????56 | ????41 | ????30 | ????18 |
| Root of Bunge Auriculate glycosides A | ????57** | ????40 | ????29 | ????11 | ????- | ????- | ????- |
| Root of Bunge Auriculate glycosides B | ????49* | ????38 | ????20 | ????8 | ????- | ????- | ????- |
| Root of Bunge Auriculate glycosides C | ????41* | ????39 | ????35 | ????32 | ????29 | ????8 | ????- |
| The new glycosides A of Root of Bunge Auriculate | ????19 | ????7 | ????- | ????- | ????- | ????- | ????- |
| The new glycosides B of Root of Bunge Auriculate | ????60** | ????55** | ????48* | ????42* | ????31 | ????18 | ????- |
| Auriculoside A glycosides A | ????54** | ????36 | ????17 | ????9 | ????- | ????- | ????- |
| Auriculoside A glycosides B | ????40* | ????25 | ????16 | ????13 | ????8 | ????- | ????- |
| The radix cynanchi bungei total saponin(e | ????38 | ????25 | ????11 | ????- | ????- | ????- | ????- |
Compare with the blank group: * P＜0.05, * * P＜0.01
(7) Root of Bunge Auriculate carbon-21 steroidal saponin(e is to the analgesic activity of mouse inflammatory pain.
1. method
Kunming mouse, body weight 18～20g, male and female half and half, animal is divided into 24 experimental group at random, 1 hydrochloric acid dolantin group and 1 blank group, 10 every group.7 carbon-21 steroidal saponin(es of experimental group ig (10mg/kg, 20mg/kg, 40mg/kg), the radix cynanchi bungei total saponin(e (50mg/kg, 100mg/kg, 200mg/kg), all (carboxymethyl cellulose, CMC) solution is made into desired concn to above medicine with the 5g/L carboxymethyl cellulose with preceding.The physiological saline of blank group ig respective volume.The continuous ig administration of each treated animal 5d, every day 1 time, the administration volume is the 0.2ml/10g body weight.The physiological saline group is identical with it.0.5h behind 1h, hydrochloric acid dolantin (20mg/kg) ig after the administration of mouse last, every mouse ig 0.6% acetate 0.2mL observes and interior each mouse of record injection acetate 20min is turned round the body number of times, compares with negative control group, judges that with the t check no difference of science of statistics is arranged.
2. result
Compare with the physiological saline group, the hydrochloric acid dolantin has good analgesic activity, and illustrative experiment is reliable.The large, medium and small dosage group of carbon-21 steroidal saponin(e all has obvious suppression effect (P＜0.001) to the pain (writhing response) that mouse peritoneal injection acetate causes.
Table 7 Root of Bunge Auriculate carbon-21 steroidal saponin(e suppresses the influence of rat gastric juice and gastric acid secretion
| Group | Dosage (mg/kg) | The writhing response number of times |
| Blank group hydrochloric acid dolantin group Root of Bunge Auriculate glycosides A | ????- ????20 ????10 ????20 | ????36.5±14.2 ????0.56±1.02** ????16.71±2.13* ????9.24±2.29** |
| Group | Dosage (mg/kg) | The writhing response number of times |
| Cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????60 ????100 ????200 | ????2.06±1.76** ????17.19±3.08* ????15.44±2.90* ????1.97±1.27** ????28.65±4.01 ????17.24±3.96* ????3.77±1.15** ????16.17±3.31* ????3.47±2.09** ????1.46±1.56** ????16.39±3.91* ????15.84±2.78* ????2.28±1.79** ????28.92±3.67 ????11.04±3.11* ????2.11±1.64** ????15.77±3.28* ????7.40±1.09** ????3.92±1.16** ????29.94±4.07 ????15.67±3.88* ????6.07±1.64** |
Compare with the blank group: * P＜0.05, * * P＜0.01
(8) the anti-mouse ethanol of Root of Bunge Auriculate carbon-21 steroidal saponin(e causes the effect of gastric mucosa injury.
1. method Wister rat is divided at random: ethanol model group, Root of Bunge Auriculate carbon-21 steroidal saponin(e group, normal control group, 10 every group.Root of Bunge Auriculate carbon-21 steroidal saponin(e group gives Root of Bunge Auriculate carbon-21 steroidal saponin(e group 100mg/kg, 1 time/day, totally 3 days by irritating stomach; Ethanol model group and normal control group give the water of equivalent.Fasting 24h before the experiment prohibits water 2h.2h after the perfusion in the 3rd day, ethanol model group and Root of Bunge Auriculate carbon-21 steroidal saponin(e group are only irritated stomach with ethanol 1ml/, put to death rat behind the 2h, get stomach.Get ulcer edge tissues mucous membrane, measure stomach mucous membrane lipid peroxide (LPO) content with the TBA fluorimetry.
The result respectively organize measured value with mean ± standard deviation (expression of x ± SD), difference is analyzed with the t method of inspection, there is significance P＜0.05 for difference.
The stomach mucous membrane LPO content of ethanol model group is apparently higher than normal control group (P＜0.01), and the stomach mucous membrane LPO content of Root of Bunge Auriculate carbon-21 steroidal saponin(e group is starkly lower than ethanol model group (P＜0.01).Root of Bunge Auriculate carbon-21 steroidal saponin(e can resist the stomach mucous membrane LPO rising that ethanol causes, the gastric mucosa injury that oxyradical is caused has provide protection.
Table 8 Root of Bunge Auriculate carbon-21 steroidal saponin(e is to the influence of gastric mucosa of rat LPO content
| Group | Dosage (mg/kg) | Stomach mucous membrane LPO content (nmol/mg) |
| Blank group ethanol model group cynauricuoside A cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????- ????100 ????100 ????100 ????100 ????100 ????100 ????100 ????100 ????100 | ??10.85±4.12 ??16.76±6.02** ??2.12±0.51**△△ ????8.62±0.63△△ ????2.03±0.45**△△ ????1.98±0.61**△△ ????9.07±1.82△△ ????1.85±0.57**△△ ????2.56±0.91**△△ ????7.48±1.52*△△ |
Compare with the blank group: * P＜0.05, * * P＜0.01; Compare with the ethanol model group: △ P＜0.05, △ △ P＜0.01
(9) effect of the anti-mercaptoethylamine inductive of Root of Bunge Auriculate carbon-21 steroidal saponin(e rat preduodenal ulcer
1. method
Male SD rat, body weight 200g, mouth is raised hydrochloric acid mercaptoethylamine 280mg/kg, administration in first day 3 times.Rat was put to death in the 3rd day.Stomach and duodenum is fixing in 10% formaldehyde solution, and the specimens paraffin embedding slices hematoxylin-eosin staining is done Histological evaluation.
2. result
Severity to duodenal ulcer mark (0-3); 0=does not have ulcer; The shallow table due to intestine erosion and ulcer of 1=; The shallow degree ulcer of 2=is often with saturating wall necrosis; 3=perforated ulcer.Each organizes measured value, and (there is significance P＜0.05 for difference for x ± SD) expression, difference t method of inspection analysis with mean ± standard deviation.
Table 9 Root of Bunge Auriculate carbon-21 steroidal saponin(e is to the influence of mercaptoethylamine inductive rat preduodenal ulcer
| Group | Dosage (mg/kg) | The scoring of duodenal ulcer severity |
| Blank group famotidine group Root of Bunge Auriculate glycosides A | ????- ????10 ????20 | ????2.85±0.92 ????0.86±0.32** ????0.92±0.31**△ |
| Group | Dosage (mg/kg) | The scoring of duodenal ulcer severity |
| Cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????20 ????20 ????20 ????20 ????20 ????20 ????20 | ?1.12±0.63△ ??0.83±0.40**△ ??0.88±0.31**△ ??1.27±1.82△ ??0.65±0.57**△△ ??1.56±0.61 ?1.48±0.52 |
Compare with the blank group: * P＜0.05, * * P＜0.01; Compare with the famotidine group: △ P＜0.05, △ △ P＜0.01
(10) Root of Bunge Auriculate carbon-21 steroidal saponin(e promotes the effect of rat stomach evacuation rate
1. method
Cleaning level Wistar rat, male and female half and half, body weight 200～300g.With the rat random packet, 8 every group, carry out modeling respectively.Control group normally fed for 4 weeks, and all the other each groups are then normally taken food whenever even-numbered days, meet the odd-numbered day fasting, all freely drink water, and add hydrochloric acid (adding 10mol/L hydrochloric acid 10ml in every premium on currency) in the water, continuous 4 weeks.Administration group rat carries out gastric infusion in the 3rd, 4 every days in week of feeding by 1ml/100g.Rats in normal control group gives distilled water, and positive controls gives 0.1% motilium suspension, totally 14 days.
2. result
Gastric emptying rate is measured.Above-mentioned rat moist forage (water mixes by 1.5: 1 with the weight ratio of the feed) adaptability of respectively organizing was raised 3 days, began experiment.Fasting be can't help giving 5g moist forage behind the water 20h, put to death animal behind the 30min, cut the abdominal cavity rapidly open, ligation stomach orifice of the stomach and pylorus are got stomach, wipe away with filter paper and to weigh after doing, cut off body of stomach along greater gastric curvature then, the flush away gastric content is also wiped away to do and is weighed, is residue weight in the stomach with the difference of weighing for forward and backward twice, the difference of eating residue weight in feed weight and the stomach then is the weight of emptying, measures the per-cent that emptying food weight accounts for the feed weight of eating and is gastric emptying rate.
Each organizes measured value, and (there is significance P＜0.05 for difference for x ± SD) expression, difference t method of inspection analysis with mean ± standard deviation.
Table 10 Root of Bunge Auriculate carbon-21 steroidal saponin(e is to the 30min gastric emptying rate influence of rat food back
| Group | Dosage (mg/kg) | Gastric emptying rate (%) |
| Blank group motilium group Root of Bunge Auriculate glycosides A | ????- ????10 ????20 | ????32.85±9.92 ????20.86±5.32** ????25.92±8.31* |
| Group | Dosage (mg/kg) | Gastric emptying rate (%) |
| Cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????20 ????20 ????20 ????20 ????20 ????20 ????20 | ????25.12±7.63* ????24.83±0.40** ????29.88±0.31 ????23.27±1.82** ????23.65±0.57** ????25.56±0.61* ????29.48±0.52 |
Compare with the blank group: * P＜0.05, * * P＜0.01
(11) Root of Bunge Auriculate carbon-21 steroidal saponin(e promotes the effect of rat intestine wriggling
1. method
100 of female Kunming mouses are divided into 10 groups according to body weight at random with mouse, 10 every group.If negative control group, intestinal peristalsis suppress model control group, Root of Bunge Auriculate saponin(e group.Animal ad lib, drinking-water.
2. observation index and result
When experiment the 0th day and the 9th day, weigh in.Prepared Chinese ink propelling rate.Began the back the 9th day in experiment, each is organized mouse and stops eating behind the 24h, negative control group gives distilled water and irritates stomach, other are respectively organized mouse and give compound diphenoxylate filling stomach (5mgPkgBW), after giving compound diphenoxylate 30min, each is organized mouse and gives prepared Chinese ink filling stomach respectively, irritates the stomach amount and is 014mLP20gBW, takes off cervical vertebra immediately and put to death animal after irritating stomach 25min, open the abdominal cavity and separate mesentery, the clip upper end is from pylorus, the lower end places on the pallet to the intestinal tube of ileocecus, gently small intestine is pulled into straight line, measure intestinal tube length " small intestine total length ", from pylorus to prepared Chinese ink forward position is " prepared Chinese ink propelling length ", calculates prepared Chinese ink propelling rate, and calculation formula is as follows:
Prepared Chinese ink propelling rate (%)=prepared Chinese ink advances length (cm)/small intestine total length (cm) * 100%
Table 11 Root of Bunge Auriculate carbon-21 steroidal saponin(e is to the influence of mouse prepared Chinese ink propelling rate
| Group | Number of animals | Small intestine total length (cm) | Prepared Chinese ink advances length (cm) | Prepared Chinese ink propelling rate (%) |
| Negative control group model control group cynauricuoside A cynauricuoside B cynauricuoside C cynanauriculoside A cynanauriculoside B cynanchum auriculatum Royle glycosides A | ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 | ????47.5±3.9 ????51.2±5.1 ????49.3±6.2 ????47.5±8.5 ????49.4±4.8 ????46.6±9.6 ????48.1±6.4 ????49.3±6.2 | ??32.7±2.1 ??17.6±2.7 ??22.0±5.6 ??23.2±4.6 ??20.0±5.7 ??21.8±4.5 ??22.0±5.6 ??22.0±5.6 | ??69.3±6.5 ??34.8±6.8 ??43.5±11.4* ??49.0±12.3**△△ ????40.2±9.6 ??47.8±10.5**△ ????45.6±9.3*△ ????43.5±11.4* |
| Group | Number of animals | Small intestine total length (cm) | Prepared Chinese ink advances skin (cm) | Prepared Chinese ink propelling rate (%) |
| Auriculoside A glycosides B radix cynanchi bungei total saponin(e | ??10 ??10 | 47.5±8.5 49.4±4.8 | 23.2±4.6 20.0±5.7 | ??49.0±12.3**△△ ????40.2±9.6 |
*, * * represents that comparing difference with model control group has significance (* P＜0.05, * * P＜0.01); △, △ △ represent that comparing difference with the blank group has significance (△ P＜0.05, △ △ P＜0.01).
The effect of (12) Root of Bunge Auriculate carbon-21 steroidal saponin(e Chinese People's Anti-Japanese Military and Political College mouse superficial gastritis
1. method
100 of male Wister rats are about body weight 300g.Mouse is divided into 10 groups at random.If negative control group, famotidine control group, Root of Bunge Auriculate saponin(e group.Fasting 24h before the experiment.Each organizes in accordance with regulations that dosage gives medicine, and negative control group gives and the isopyknic distilled water of administration group.Under waking state, the aspirin solution with 20mmol/L gavages by the 100mg/kg per os respectively.Behind the 4h,, cut open inspection, acute diffuse inflammation pathology in the visible stomach with sacrifice of animal.
2. observation index and result
Observe what, size and distribution position thereof of gastric bleeding kitchen range with dissecting microscope.Measure the major diameter of each hemorrhagic focus, ask its summation, compare as bleeding index.Data are with mean ± standard deviation (x ± SD) expression.According to every group of bleeding index of gained, press the calculation formula of gastrorrhagia inhibiting rate: hemorrhage inhibiting rate=[(control group index-administration class index)/control group index] * 100%; Calculate the gastrorrhagia inhibiting rate.The relatively employing t check of each group difference.
7 carbon-21 steroidal saponin(es of table 12 ig and radix cynanchi bungei total saponin(e are to the influence of rat superficial gastritis
| Group | Dosage (mg/kg) | Number of animals | Bleeding index | Hemorrhage inhibiting rate (%) |
| Blank famotidine group cynauricuoside A cynauricuoside B cynauricuoside C cynanauriculoside A | ???- ???100 ???10 ???20 ???40 ???10 ???20 ???40 ???10 ???20 ???40 ???10 ???20 ???40 | ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 | ????47.24±7.00 ????8.21±4.01** ????25.09±8.71* ????18.63±4.69** ????11.26±6.75** ????28.69±5.18* ????24.44±7.61* ????12.76±6.77** ????32.69±9.21 ????26.44±6.40* ????13.06±6.17** ????22.55±8.71* ????13.27±4.39** ????10.96±7.05** | ????- ????85.94** ????46.89* ????62.96** ????89.01** ????44.15* ????53.33* ????81.09** ????38.25 ????48.65* ????75.24** ????56.13* ????74.51** ????80.16** |
| Group | Dosage (mg/kg) | Number of animals | Bleeding index | Hemorrhage inhibiting rate (%) |
| Cynanauriculoside B cynanchum auriculatum Royle glycosides A cynanchum auriculatum Royle glycosides B radix cynanchi bungei total saponin(e | ????10 ????20 ????40 ????10 ????20 ????40 ????10 ????20 ????40 ????50 ????100 ????200 | ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 ????10 | ????26.49±7.01* ????20.54±7.91* ????12.06±5.25** ????31.32±8.85 ????24.64±8.69* ????12.06±6.24** ????24.75±6.51* ????15.44±4.69** ????10.22±6.35** ????30.44±8.06 ????25.07±6.19* ????13.06±8.07** | ??48.63* ??51.97* ??76.35** ??37.89 ??51.48* ??76.69** ??51.84* ??69.24** ??79.09** ??38.14 ??49.56* ??73.37** |
Compare with the blank group: * P＜0.05, * * P＜0.01
Embodiment
Embodiment 1:
Preparation radix cynanchi bungei total saponin(e
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract chloroform heating in water bath 2 hours, cooled and filtered, reclaim under reduced pressure chloroform, get chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times, each 0.5 hour, get the insoluble part of normal hexane, i.e. radix cynanchi bungei total saponin(e.
The radix cynanchi bungei total saponin(e, light brown powder, Lieberman-Burchard and Keller-Killiani reaction all are positive, and show to be all the steroidal compounds that contains the 2-desoxy sugar.
Embodiment 2:
Preparation Root of Bunge Auriculate glycosides A
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract is used chloroform heating in water bath 2 hours, cooled and filtered, the reclaim under reduced pressure chloroform gets chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times each 0.5 hour, gets the insoluble part of normal hexane.The insoluble part of normal hexane is carried out silica gel column chromatography, carry out gradient elution, check the chromatography flow point with thin-layer chromatography with chloroform-ethanol, flow point with identical single spot merges, concentrate, get flow point 1,2,3,4,5,6, wherein flow point 2 is through HPLC (MeOH: H
2O) separation, purifying obtain Root of Bunge Auriculate glycosides A.
Root of Bunge Auriculate glycosides A (cynauricuoside A), white amorphous powder, mp167-173 ℃, [α]
D 28:-28.63 ° of (c=0.52, CHCl
3), molecular formula: C
84H
98O
24Measure through spectroscopic data analysis and physicochemical character that (12 (2): Root of Bunge Auriculate glycosides A 197-210) is in full accord for Chen Jijun etc., Yunnan plant research .1990 with bibliographical information.
Embodiment 3:
Preparation Root of Bunge Auriculate glycosides B
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract is used chloroform heating in water bath 2 hours, cooled and filtered, the reclaim under reduced pressure chloroform gets chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times each 0.5 hour, gets the insoluble part of normal hexane.The insoluble part of normal hexane is carried out silica gel column chromatography, carry out gradient elution, check the chromatography flow point with thin-layer chromatography with chloroform-ethanol, flow point with identical single spot merges, concentrate, get flow point 1,2,3,4,5,6, wherein flow point 2 is through HPLC (MeOH: H
2O) separation, purifying obtain Root of Bunge Auriculate glycosides B.
Root of Bunge Auriculate glycosides B (cynauricuoside B), white amorphous powder, mp137-142 ℃, [α]
D 28:-64.96 ° of (c=0.51, CHCl
3), molecular formula: C
52H
82O
19Measure through spectroscopic data analysis and physicochemical character that (12 (2): Root of Bunge Auriculate glycosides B 197-210) is in full accord for Chen Jijun etc., Yunnan plant research .1990 with bibliographical information.
Embodiment 4:
Preparation Root of Bunge Auriculate glycosides C
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract is used chloroform heating in water bath 2 hours, cooled and filtered, the reclaim under reduced pressure chloroform gets chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times each 0.5 hour, gets the insoluble part of normal hexane.The insoluble part of normal hexane is carried out silica gel column chromatography, carry out gradient elution with chloroform-ethanol, check the chromatography flow point with thin-layer chromatography, flow point with identical single spot merges, concentrate, get flow point 1,2,3,4,5,6, wherein (MeOH: H2O) separation, purifying obtain Root of Bunge Auriculate glycosides C to flow point 3 through HPLC.
Root of Bunge Auriculate glycosides C (cynauricuoside C), white amorphous powder, mp174-181 ℃, [α]
D 28:-25.15 ° of (c=0.32, CHCl
3), molecular formula: C
68H
110O
29Measure through spectroscopic data analysis and physicochemical character that (12 (2): Root of Bunge Auriculate glycosides C 197-210) is in full accord for Chen Jijun etc., Yunnan plant research .1990 with bibliographical information.
Embodiment 5:
The new glycosides A of preparation Root of Bunge Auriculate
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract is used chloroform heating in water bath 2 hours, cooled and filtered, the reclaim under reduced pressure chloroform gets chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times each 0.5 hour, gets the insoluble part of normal hexane.The insoluble part of normal hexane is carried out silica gel column chromatography, carry out gradient elution, check the chromatography flow point with thin-layer chromatography with chloroform-ethanol, flow point with identical single spot merges, concentrate, get flow point 1,2,3,4,5,6, wherein flow point 4 is through HPLC (MeOH: H
2O) separation, purifying obtain the new glycosides A of Root of Bunge Auriculate.
The new glycosides A of Root of Bunge Auriculate (cynanauriculoside A), white amorphous powder, mp:172-176 ℃, [α]
D 28: 0 ° (c=0.80, EtOH), molecular formula: C
55H
88O
20Through spectroscopic data analysis and physicochemical character measure with bibliographical information (Zhang Rusong etc., the composition Study of Root of Bunge Auriculate extracorporeal suppression tumor cell. Acta Pharmaceutica Sinica, 2000,35 (6): new glycosides A is in full accord for Root of Bunge Auriculate 431-437).
Embodiment 6:
The new glycosides B of preparation Root of Bunge Auriculate
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract is used chloroform heating in water bath 2 hours, cooled and filtered, the reclaim under reduced pressure chloroform gets chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times each 0.5 hour, gets the insoluble part of normal hexane.The insoluble part of normal hexane is carried out silica gel column chromatography, carry out gradient elution, check the chromatography flow point with thin-layer chromatography with chloroform-ethanol, flow point with identical single spot merges, concentrate, get flow point 1,2,3,4,5,6, wherein flow point 5 is through HPLC (MeOH: H
2O) separation, purifying obtain Root of Bunge Auriculate glycosides B.
The new glycosides B of Root of Bunge Auriculate (cynanauriculoside B), white amorphous powder, mp:174-177 ℃, [α]
D 28:+11.2 ° (c=0.50, EtOH), molecular formula: C
54H
86O
21Through spectroscopic data analysis and physicochemical character measure with bibliographical information (Zhang Rusong etc., the composition Study of Root of Bunge Auriculate extracorporeal suppression tumor cell. Acta Pharmaceutica Sinica, 2000,35 (6): new glycosides B is in full accord for Root of Bunge Auriculate 431-437).
Embodiment 7:
Preparation Auriculoside A glycosides A
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract is used chloroform heating in water bath 2 hours, cooled and filtered, the reclaim under reduced pressure chloroform gets chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times each 0.5 hour, gets the insoluble part of normal hexane.The insoluble part of normal hexane is carried out silica gel column chromatography, carry out gradient elution, check the chromatography flow point with thin-layer chromatography with chloroform-ethanol, flow point with identical single spot merges, concentrate, get flow point 1,2,3,4,5,6, wherein flow point 6 is through HPLC (MeOH: H
2O) separation, purifying obtain Auriculoside A glycosides A.
Auriculoside A glycosides A, white amorphous powder, mp151-154 ℃, [α]
D 28:-32.1 ° (c=0.04, EtOH), molecular formula: C
60H
100O
24Through spectroscopic data analysis and physicochemical character measure with the patent record (Zhang Rusong, Ye Yiping. extraction separation has the novel carbon-21 steroidal saponin(e of antitumor action from Root of Bunge Auriculate. the patent No.: Auriculoside A glycosides A 00136364.6) is in full accord.
Embodiment 8:
Preparation Auriculoside A glycosides B
After Root of Bunge Auriculate dried root 10kg pulverizes, with 90% alcohol reflux 3 times, each 2 hours, united extraction liquid, decompression and solvent recovery gets ethanol extraction, this extract is used chloroform heating in water bath 2 hours, cooled and filtered, the reclaim under reduced pressure chloroform gets chloroform extract, again with in the chloroform extract impouring normal hexane, reflux 2 times each 0.5 hour, gets the insoluble part of normal hexane.The insoluble part of normal hexane is carried out silica gel column chromatography, carry out gradient elution, check the chromatography flow point with thin-layer chromatography with chloroform-ethanol, flow point with identical single spot merges, concentrate, get flow point 1,2,3,4,5,6, wherein flow point 6 is through HPLC (MeOH: H
2O) separation, purifying obtain Auriculoside A glycosides B.
Auriculoside A glycosides B, white amorphous powder, mp141-146 ℃, [α]
D 28:+4.4 ° (c=0.16, EtOH), molecular formula: C
61H
98O
24Through spectroscopic data analysis and physicochemical character measure with the patent record (Zhang Rusong, Ye Yiping. extraction separation has the novel carbon-21 steroidal saponin(e of antitumor action from Root of Bunge Auriculate. the patent No.: Auriculoside A glycosides B 00136364.6) is in full accord.
Embodiment 9:
Get Root of Bunge Auriculate glycosides A100mg,,,, promptly get the injection lyophilized powder according to conventional freeze-dry process freeze-drying with N.F,USP MANNITOL 200mg with an amount of water for injection dissolving.Be used for the treatment of gastrointestinal tract disease.
Embodiment 10:
The radix cynanchi bungei total saponin(e is disperseed with an amount of water for injection, and spraying drying or vacuum-drying get radix cynanchi bungei total saponin(e dry powder, and taking polyethylene glycol 400 adds radix cynanchi bungei total saponin(e dry powder, and the limit edged is stirred to even, adopts pressing, makes soft capsule.Be used for the treatment of gastrointestinal tract disease.
Embodiment 11:
Get radix cynanchi bungei total saponin(e 100g, disperse with an amount of water for injection, add right amount of auxiliary materials, mixing is made particle, and drying is pressed into 1000, and sugar coating promptly gets radix cynanchi bungei total saponin(e sheet.Be used for the treatment of gastrointestinal tract disease.
Claims (7)
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| CN1152044C (en) * | 2000-12-16 | 2004-06-02 | 浙江省医学科学院 | Extraction and separation of novel carbon-21 steroidal glycosides with antitumor effects from Baishouwu |
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| CN113075325A (en) * | 2021-03-30 | 2021-07-06 | 贵州医科大学 | Method for simultaneously measuring contents of 8 index components in Miao medicine radix cynanchi wilfordii |
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| CN116585366A (en) * | 2022-05-17 | 2023-08-15 | 湖南中嘉生物医药有限公司 | Radix cynanchi bungei extract and application thereof |
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